METHOD FOR PRODUCING POLYALKYLENE GLYCOL DERIVATIVE HAVING AMINO GROUP AT END
    11.
    发明申请
    METHOD FOR PRODUCING POLYALKYLENE GLYCOL DERIVATIVE HAVING AMINO GROUP AT END 审中-公开
    生产具有氨基的聚亚甲基甘氨酸衍生物的方法

    公开(公告)号:US20160159831A1

    公开(公告)日:2016-06-09

    申请号:US14959088

    申请日:2015-12-04

    摘要: A method simply produces a narrowly distributed and high-purity polyalkylene glycol derivative having an amino group at an end without using a heavy metal catalyst. A method for producing a polyalkylene glycol derivative having an amino group at the end by reacting a compound represented by the general formula (V) with an alkylene oxide, then reacting a reaction product with an electrophile represented by the general formula (I), and deprotecting the obtained product without using a heavy metal: RA3O(RA4O)k-1RA4O−M+  (V) wherein RA3 represents a linear; branched, or cyclic hydrocarbon group having 1 to 20 carbon atoms; RA4 represents an alkylene group having 2 to 8 carbon atoms; k represents an integer of 2 to 5; and M represents an alkali metal; wherein RA1a and RA1b each independently represent a protective group of the amino group, or one of RA1a and RA1b represents H and the other represents a protective group of the amino group, or RA1a and RA1b bind to each other to form a cyclic protective group, and the protective group is deprotectable without using a heavy metal; RA2 represents a linear, branched, or cyclic hydrocarbon group having 1 to 6 carbon atoms; and X represents a leaving group.

    摘要翻译: 一种方法简单地产生在不使用重金属催化剂的情况下在末端具有氨基的窄分布且高纯度的聚亚烷基二醇衍生物。 通过使由通式(V)表示的化合物与烯化氧反应,然后使反应产物与通式(I)表示的亲电子试剂反应,以及通式 不使用重金属使得到的产物脱保护:RA3O(RA4O)k-1RA4O-M +(V)其中RA3表示直链; 具有1〜20个碳原子的支链或环状烃基; RA4表示碳原子数2〜8的亚烷基。 k表示2〜5的整数, M表示碱金属; 其中RA1a和RA1b各自独立地表示氨基的保护基,或者RA1a和RA1b之一表示H,另一个表示氨基的保护基,或RA1a和RA1b彼此结合形成环保护基, 并且保护基团在不使用重金属的情况下可脱保护; RA2表示碳原子数1〜6的直链状,支链状或环状的烃基。 X表示离去基团。

    Method for producing polyalkylene glycol derivative having amino group at end

    公开(公告)号:US10550136B2

    公开(公告)日:2020-02-04

    申请号:US16454552

    申请日:2019-06-27

    摘要: A method simply produces a narrowly distributed and high-purity polyalkylene glycol derivative having an amino group at an end without using a heavy metal catalyst. A method for producing a polyalkylene glycol derivative having an amino group at the end by reacting a compound represented by the general formula (V) with an alkylene oxide, then reacting a reaction product with an electrophile represented by the general formula (I), and deprotecting the obtained product without using a heavy metal: RA3O(RA4O)k−1RA4O−M+  (V) wherein RA3 represents a linear, branched, or cyclic hydrocarbon group having 1 to 20 carbon atoms; RA4 represents an alkylene group having 2 to 8 carbon atoms; k represents an integer of 2 to 5; and M represents an alkali metal: wherein RA1a and RA1b each independently represent a protective group of the amino group, or one of RA1a and RA1b represents H and the other represents a protective group of the amino group, or RA1a and RA1b bind to each other to form a cyclic protective group, and the protective group is deprotectable without using a heavy metal; RA2 represents a linear, branched, or cyclic hydrocarbon group having 1 to 6 carbon atoms; and X represents a leaving group.

    METHOD FOR PRODUCING POLYALKYLENE GLYCOL DERIVATIVE HAVING AMINO GROUP AT END

    公开(公告)号:US20190315777A1

    公开(公告)日:2019-10-17

    申请号:US16454552

    申请日:2019-06-27

    摘要: A method simply produces a narrowly distributed and high-purity polyalkylene glycol derivative having an amino group at an end without using a heavy metal catalyst. A method for producing a polyalkylene glycol derivative having an amino group at the end by reacting a compound represented by the general formula (V) with an alkylene oxide, then reacting a reaction product with an electrophile represented by the general formula (I), and deprotecting the obtained product without using a heavy metal: RA3O(RA4O)k-1RA4O−M+  (V) wherein RA3 represents a linear, branched, or cyclic hydrocarbon group having 1 to 20 carbon atoms; RA4 represents an alkylene group having 2 to 8 carbon atoms; k represents an integer of 2 to 5; and M represents an alkali metal: wherein RA1a and RA1b each independently represent a protective group of the amino group, or one of RA1a and RA1b represents H and the other represents a protective group of the amino group, or RA1a and RA1b bind to each other to form a cyclic protective group, and the protective group is deprotectable without using a heavy metal; RA2 represents a linear, branched, or cyclic hydrocarbon group having 1 to 6 carbon atoms; and X represents a leaving group.